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US 6,333,330 B1Granted
Pyrazolopyrimidinone CGMP PDE5 inhibitors for the treatment of sexual dysfunction
AssigneePfizer Inc.
InventorsMark Edward Bunnage, John Paul Mathias, Graham Nigel Maw, David James Rawson, Stephen Derek Albert Street, Anthony Wood
Life of this patent
Estimating the term…
Abstract
There is provided compounds of formula IA and of formula IB, wherein R1, R2, R3, R4 and A have meanings given in the description, which are useful in the curative and prophylactic treatment of medical conditions for which inhibition of a cyclic guanosine 3′,5′-monophosphate phosphodiesterase (e.g. cGMP PDE5) is desired.
Claims11
A compound of formula IA, or of formula IB:
- wherein
- A represents CH or N;
- R1 represents H, lower alkyl, Het, alkylHet, aryl or alkylaryl, which latter five groups are all optionally substituted (and/or, in the case of lower alkyl, optionally terminated) by one or more substituents selected from halo, cyano, nitro, lower alkyl, OR5, C(O)R6, C(O)OR7, C(O)NR8R9, NR10aR10b and SO2NR11aR11b;
- R2 represents C(O)NR12R13, C(O)OR12, NR12R13, N(H)SO2R12, N(H)SO2NR12R13,
- N(H)C(O)R12, OR12a, lower alkyl (which alkyl group is interrupted by one or more of O, S or N(R12) and/or substituted or terminated by C(O)NR12R13, C(O)OR12 or aryl or Het1), cyano, aryl or Het1, provided that, in a compound of formula IA wherein R2 is alkoxy, A must be N;
- R3, R12 and R13 independently represent H or lower alkyl, which alkyl group is optionally substituted and/or optionally terminated by one or more substituents selected from aryl,
- Het, halo, cyano, nitro, OR5, C(O)R6, C(O)OR7, C(O)NR8R9, NR10aR10b and
- SO2N11aR11b;
- R4 represents SO2NR14R15;
- R14 and R15, together with the nitrogen to which they are attached, form Het;
- Het represents an optionally substituted four- to twelve-membered heterocyclic group, which group contains at least one nitrogen atom and, optionally, one or more further heteroatoms selected from nitrogen, oxygen and sulphur;
- Het1 represents an optionally substituted four- to twelve-membered heterocyclic group, which group contains at least one nitrogen atom or at least one oxygen atom and, optionally, one or more further heteroatoms selected from nitrogen, oxygen and sulphur;
- and
- R5, R6, R7, R8, R9, R11a, R11b and R12a independently represent, at each occurrence when used herein, H or lower alkyl;
- R10a and R10b, at each occurrence when used herein, either independently represent, H or lower alkyl or, together with the nitrogen atom to which they are attached, represent azetidinyl, pyrollidinyl or piperidinyl;
- or a pharmaceutically, or a veterinarily, acceptable derivative thereof.
13 more elements
Dependencies are inferred from the claim text.